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α2A receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) Adrenergic Receptor (24) Apoptosis (1) Dopamine Receptor (3) Histamine Receptor (2) Isotope-Labeled Compounds (2) mAChR (1) MCHR1 (GPR24) (1) Trace Amine-associated Receptor (TAAR) (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (7) Endocrinology (11) Inflammation/Immunology (1) Metabolic Disease (4) Neurological Disease (14)

Inhibitors & Agonists

Peptides

Recombinant Proteins

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17416

Guanfacine hydrochloride 1 Publications Verification	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

HY-U00123A

Guanoxabenz hydrochloride Hydroxyguanabenz hydrochloride	Adrenergic Receptor	Neurological Disease
Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a K_i of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor .

HY-U00117

Lusaperidone R107474	Adrenergic Receptor	Neurological Disease Endocrinology
Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with K_is of 0.13 and 0.15 nM for α2A and α2C, respectively.

HY-17416A

Guanfacine	Adrenergic Receptor	Neurological Disease Endocrinology
Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

HY-17416S2

Guanfacine-13C,d5 hydrochloride	Adrenergic Receptor Isotope-Labeled Compounds	Cardiovascular Disease Endocrinology
Guanfacine- ¹³C,d₅ hydrochloride is the deuterium and ¹³C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

HY-17416R

Guanfacine hydrochloride (Standard)	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanfacine (hydrochloride) (Standard) is the analytical standard of Guanfacine (hydrochloride). This product is intended for research and analytical applications. Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

HY-17416AS1

Guanfacine-15N3,13C2	Adrenergic Receptor Isotope-Labeled Compounds	Neurological Disease Endocrinology
Guanfacine- ¹⁵N₃, ¹³C₂ is ¹⁵N and ¹³C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

HY-162620

α2A-AR agonist 1	Adrenergic Receptor	Cancer
α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC₅₀ of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED₅₀ of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .

HY-U00123

Guanoxabenz Hydroxyguanabenz	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanoxabenz is an α2 adrenergic receptor agonist, with a K_i of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor .

HY-105699

Napamezole	Adrenergic Receptor	Neurological Disease
Napamezole is an **α_2A adrenergic receptor** antagonist and a serotonin/norepinephrine uptake inhibitor. Napamezole increases the levels of monoamines in the brain by blocking monoamine uptake, which gives it antidepressant activity .

HY-17416AS

Guanfacine-13C,15N3	Adrenergic Receptor	Neurological Disease
Guanfacine- ¹³C, ¹⁵N₃ is the ¹³C and ¹⁵N labeled Guanfacine[1]. Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)[2][3][4].

HY-12716

BRL-44408	Adrenergic Receptor	Endocrinology
BRL-44408 is a selective adrenergic receptor antagonist of α2A/α2B AR. BRL-44408 can effectively antagonize the inhibitory effects of norepinephrine or adrenergic receptor agonist Clonidine (HY-12721) on K ⁺-induced [3H]norepinephrine and [3H]5-hydroxytryptamine release. BRL-44408 has a higher affinity for human platelet membranes containing α2A-adrenoceptors than BRL-41992 and Imiloxan (HY-101337). BRL-44408 may affect the release of norepinephrine and 5-hydroxytryptamine through a mechanism mediated by α2A-adrenoceptors, and has a potential role in the regulation of neurotransmitter release .

HY-100300

AGN 192836	Adrenergic Receptor	Cardiovascular Disease Endocrinology
AGN 192836 is a potent and selective α2 adrenergic agonist with EC₅₀s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

HY-U00244

Benzquinamide P2647; BZQ; Benzoquinamide	Adrenergic Receptor	Metabolic Disease Endocrinology
Benzquinamide (P2647) is an antiemetic which can bind to the *α_2A, α_2B, and α_2C* adrenergic receptors (α2-AR) with K_i values of 1,365, 691, and 545 nM, respectively.

HY-116031

ATC0175 free base	MCHR1 (GPR24)	Others
ATC0175 (free base) is a potent and selective antagonist of melanin-concentrating hormone receptor 1 (MCH-R1) with an IC₅₀ value of 3.4 nM, as well as good selectivity over the Y5 and the **α_2A receptors**. ATC0175 (free base) is promising for research of obesity .

HY-101610

OPC-28326	Adrenergic Receptor	Cardiovascular Disease Endocrinology
OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with K_i of 2040, 285, and 55?nM for α2A-, α2B- and α2C-adrenoceptors, respectively.

HY-W909149

TAAR1 agonist 3	Trace Amine-associated Receptor (TAAR) Adrenergic Receptor	Neurological Disease
TAAR1 agonist 3 is a trace amine-associated receptor 1 (TAAR1) agonist (pEC₅₀=7.6). TAAR1 agonist 3 is also a full agonist of the **α_2A receptor (pEC₅₀**=6). TAAR1 agonist 3 can be used in the study of neuropsychiatric diseases .

HY-103216

RWJ52353	Adrenergic Receptor	Neurological Disease
RWJ52353 is a selective, orally active ligand for α2D adrenoceptor, which binds α2D, α2A, α2B and α1 receptors, with K_is of 1.5, 254, 621 and 443 nM. RWJ52353 exhibits analgesic efficacy in mouse abdominal irritation test (MAIT), with an ED₅₀ of 15.1 mg/kg .

HY-U00244A

Benzquinamide hydrochloride P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride	Adrenergic Receptor	Cancer
Benzquinamide (P2647) is an antiemetic which can bind to the *α_2A, α_2B, and α_2C* adrenergic receptors (α2-AR) with K_i values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .

HY-14689

Ecopipam hydrochloride SCH 39166 hydrochloride	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with K_is of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (K_i=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity .

HY-14690

Ecopipam SCH 39166	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
Ecopipam (SCH 39166) is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with K_is of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (K_i=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia and obesity .

HY-101198

Clobenpropit dihydrobromide	Histamine Receptor Apoptosis	Neurological Disease Cancer
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC₅₀ of 8.07 for histamine H3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (K_i 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (K_i 7.4 nM) and α2A/α2C adrenoceptors (K_i 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .

HY-110033

Ecopipam hydrobromide SCH 39166 hydrobromide	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
Ecopipam (SCH 39166) hydrobromide is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with K_is of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (K_i=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrobromide can be used for the research of schizophrenia and obesity .

HY-12709A

ARC 239 dihydrochloride	Adrenergic Receptor	Cardiovascular Disease Inflammation/Immunology
ARC 239 dihydrochloride is a selective α2B/2C adrenoceptor antagonist (pK_d values are 5.95, 7.41 and 7.56 at α2A, α2B, and α2C receptors respectively). ARC 239 dihydrochloride binds to CHO cell membranes expressing human recombinant a2A-, a2B- or a2C-adrenoceptor subtypes with pK_is of 5.6, 8.4, and 7.08, respectively .

HY-P5846

Muscarinic toxin 3 MT3	mAChR Adrenergic Receptor	Neurological Disease
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC₅₀s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M₁, M₄, α_1A, α_1B, α_1D,α_2A,α_2B and α_2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .

HY-117046A

AVN-101 hydrochloride	5-HT Receptor Histamine Receptor Adrenergic Receptor	Neurological Disease
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (K_i values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .

Cat. No.	Product Name	Target	Research Area

HY-P5846

Muscarinic toxin 3 MT3	mAChR Adrenergic Receptor	Neurological Disease
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC₅₀s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M₁, M₄, α_1A, α_1B, α_1D,α_2A,α_2B and α_2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .

Cat. No.	Compare	Product Name	Species	Source

HY-P702203

	ADRA2A-VLPs Protein, Human (HEK293, His) Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2AAR	Human	HEK293
	ADRA2A-VLPs Protein, Human (HEK293, His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P701236.

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Cat. No.	Product Name	Chemical Structure

HY-17416S2

Guanfacine-13C,d5 hydrochloride
Guanfacine- ¹³C,d₅ hydrochloride is the deuterium and ¹³C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

Guanfacine-13C,d5 hydrochloride

Guanfacine- ¹³C,d₅ hydrochloride is the deuterium and ¹³C labeled Guanfacine hydrochloride (HY-17416). Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

HY-17416AS1

Guanfacine-15N3,13C2
Guanfacine- ¹⁵N₃, ¹³C₂ is ¹⁵N and ¹³C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

Guanfacine-15N3,13C2

Guanfacine- ¹⁵N₃, ¹³C₂ is ¹⁵N and ¹³C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .

HY-17416AS

Guanfacine-13C,15N3
Guanfacine- ¹³C, ¹⁵N₃ is the ¹³C and ¹⁵N labeled Guanfacine[1]. Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)[2][3][4].

Guanfacine-13C,15N3

Guanfacine- ¹³C, ¹⁵N₃ is the ¹³C and ¹⁵N labeled Guanfacine[1]. Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD)[2][3][4].

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